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评价海藻酸和海藻酸钙的超级崩解剂功能,用于设计口腔分散片。

Evaluation of the super disintegrant functionnalities of alginic acid and calcium alginate for the design of orodispersible mini tablets.

机构信息

UMR 5253, Equipe MACS, ICGM, University of Montpellier, Montpellier, France; Department of Pharmacy, Nîmes University Hospital, Nimes, France.

UMR 5253, Equipe MACS, ICGM, University of Montpellier, Montpellier, France.

出版信息

Carbohydr Polym. 2018 Oct 1;197:576-585. doi: 10.1016/j.carbpol.2018.06.002. Epub 2018 Jun 6.

Abstract

This study explores the influence of different synthesis methods and drying conditions in the preparation of sodium alginate-derivate xerogels presenting interesting disintegrant functionalities. Xerogels containing alginic acid (AA) or calcium alginate (CaA) and a mixture of both, AA/CaA, were isolated using two different drying methods oven and rotary evaporation. AA showed the best wettability behavior, in contrast to the rigid crosslinked CaA structure which showed a limited rate of water penetration. Interestingly, xerogel containing AA dried in the oven showed an enhanced maximum water uptake. Oven drying seems to favor the isolation of materials presenting good tabletability. Compression parameters of the formulations (tensile strength, elastic energy and porosity) were not affected by their presence (5%) in the design of OroDispersible Mini Tablets. In vitro disintegration results highlighted the water wicking as the key factor leading the disintegration mechanism of these materials. These results show promise of potential properties for the development of super disintegrant excipients.

摘要

本研究探讨了不同合成方法和干燥条件对具有有趣崩解剂功能的海藻酸钠衍生物干凝胶制备的影响。使用两种不同的干燥方法——烘箱干燥和旋转蒸发法,分离出含有藻酸(AA)或钙藻酸盐(CaA)以及两者混合物(AA/CaA)的干凝胶。AA 表现出最佳的润湿性,而刚性交联的 CaA 结构则表现出有限的水分渗透速率。有趣的是,在烘箱中干燥的含有 AA 的干凝胶表现出增强的最大吸水率。烘箱干燥似乎有利于分离出具有良好可压性的材料。配方的压缩参数(拉伸强度、弹性能量和孔隙率)不受其存在(5%)的影响,这些参数被设计为 OroDispersible Mini Tablets。体外崩解结果突出了水分吸湿性作为导致这些材料崩解机制的关键因素。这些结果显示了开发超级崩解剂辅料的潜在特性。

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